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United States Patent | 6,107,320 |
Murugesan ,   et al. | August 22, 2000 |
Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R.sup.1, R.sup.2 and R.sup.3 are each independently (a) hydrogen, except that R.sup.1 is other than hydrogen; (b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ; (c) halo; (d) hydroxyl; (e) cyano; (f) nitro; (g) --C(O)H or --C(O)R.sup.6 ; (h) --CO.sub.2 H or --CO.sub.2 R.sup.6 ; (i) --SH, --S(O).sub.n R.sup.6, --S(O).sub.m --OH, --S(O).sub.m --OR.sup.6, --O--S(O).sub.m --R.sup.6, --O--S(O).sub.m OH or --O--S(O).sub.m --OR.sup.6 ; (j) --Z.sup.4 --NR.sup.7 R.sup.8 ; or (k) --Z.sup.4 --N(R.sup.11)--Z.sup.5 --NR.sup.9 R.sup.10 ; and the remaining symbols are as defined in the specification.
Inventors: | Murugesan; Natesan (Lawrenceville, NJ); Hunt; John T. (Princeton, NJ) |
Assignee: | Bristol-Myers Squibb Co. (Princeton, NJ) |
Appl. No.: | 584767 |
Filed: | January 11, 1996 |
Current U.S. Class: | 514/379; 514/380; 548/241; 548/243; 548/244; 548/245; 548/246 |
Intern'l Class: | A61K 031/422; A61K 031/423; C07D 261/16; C07D 261/12 |
Field of Search: | 514/379,380 548/241,243,244,245,246 |
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5514691 | May., 1996 | Chan et al. | 514/312. |
5514696 | May., 1996 | Murugesan et al. | 514/380. |
5571821 | Nov., 1996 | Chan et al. | |
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